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TR-14035

Cat. No. M10729
TR-14035  Structure
Size Price Availability Quantity
5mg USD 220  USD220 In stock
10mg USD 330  USD330 In stock
50mg USD 880  USD880 In stock
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Quality Control & Documentation
Biological Activity

TR-14035 is an orally active α4b7/a4b1 integrins (a4b7/a4b1 integrindual inhibitors, for α4b7 和 a4b1 function IC50 The values are 7 nM and 87 nM, respectively. TR-14035 can be used for the study of inflammatory and autoimmune diseases.

Chemical Information
Molecular Weight 474.33
Formula C24H21Cl2NO5
CAS Number 232271-19-1
Form Solid
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hao Li, et al. Expert Opin Ther Pat. α 4 β 7 integrin inhibitors: a patent review

[2] Minoru Tsuda-Tsukimoto, et al. Pharm Res. Characterization of hepatobiliary transport systems of a novel alpha4beta1/alpha4beta7 dual antagonist, TR-14035

[3] M Tsuda-Tsukimoto, et al. Xenobiotica. Pharmacokinetics and metabolism of TR-14035, a novel antagonist of a4ss1/a4ss7 integrin mediated cell adhesion, in rat and dog

[4] Minoru Tsuda-Tsukimoto, et al. Drug Metab Pharmacokinet. Role of human liver cytochrome P450 2C9 in the metabolism of a novel alpha4beta1/alpha4beta7 dual antagonist, TR-14035

[5] Ila Sircar, et al. Bioorg Med Chem. Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist

Related Integrin Products
HSDVHK-NH2

HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).

LDV

LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC.

Cyclo(RADfK)

Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis.

Obtustatin

Obtustatin is a non-RGD disintegrin of 41 residues.

Integrin Binding Peptide

Integrin Binding Peptide is derived by fibronectin.

  Catalog
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Keywords: TR-14035 supplier, Integrin, inhibitors, activators


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